1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Tubulin polymerization-IN-13

Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity.

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Tubulin polymerization-IN-13 Chemical Structure

Tubulin polymerization-IN-13 Chemical Structure

CAS No. : 2426665-56-5

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Description

Tubulin polymerization-IN-13 (Compound 4f) is a tubulin polymerization inhibitor (IC50=0.37 μM). Tubulin polymerization-IN-13 shows anti-proliferative activity against cancer cells, induces apoptosis and potential antivascular activity[1].

IC50 & Target

IC50: 0.37 μM (tubulin polymerization)[1]

In Vitro

Tubulin polymerization-IN-13 (0.005-2.8 nM) treatment inhibits tumor cell proliferation[1].
Tubulin polymerization-IN-13 (8.7-10 μM) is non-toxic in non-tumor cells[1].
Tubulin polymerization-IN-13 (1-50 nM; 24 h) treatment induces cell cycle arrest in G2/M[1].
Tubulin polymerization-IN-13 (10 nM; 24 and 48 h) treatment induces cell apoptosis[1].
Tubulin polymerization-IN-13 (10-100 nM; 24 h) treatment induces alteration of the microtubule network[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: HeLa, HT-29, Daoy, HL-60, SEM, and Jurkat cells
Concentration: 0.005-2.8 nM
Incubation Time:
Result: Showed IC50s of 2.8 nM, 2.1 nM, 0.005 nM, 2.7 nM, 0.31 nM, and 0.28 nM for HeLa, HT-29, Daoy, HL-60, SEM, and Jurkat cells, respectively.

Cell Cytotoxicity Assay[1]

Cell Line: Peripheral blood lymphocytes (PBL)
Concentration: 8.7-10 μM
Incubation Time:
Result: Showed a GI50 of 8.7 μM in quiescent lymphocytes.

Cell Cycle Analysis[1]

Cell Line: HeLa cells
Concentration: 1, 5, 10, and 50 nM
Incubation Time: 24 hours
Result: Induced a G2/M arrest at 10 nM, increased G2/M cells accompanied by a strong reduction of cells in the G1 phase.

Apoptosis Analysis[1]

Cell Line: HeLa cells
Concentration: 10 nM
Incubation Time: 24 and 48 hours
Result: Induced caspase-9 activation, PARP cleavage, Bcl-2 phosphorylation and Mcl-1 downregulation.

Immunofluorescence[1]

Cell Line: HeLa cells
Concentration: 10, 50, and 100 nM
Incubation Time: 24 hours
Result: Showed the disorganization of microtubules at 10 nM, and much more evident at 50 and 100 nM.
In Vivo

Tubulin polymerization-IN-13 (intraperitoneal injection; 15 or 5 mg/kg; once every other day; 4 times) reduces tumor growth in a dose-dependent manner in an orthotopic murine tumor model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Seven-week-old C57BL/6 female mice orthotopically injected into the mammary fat pad with E0771 mammary carcinoma cells[1]
Dosage: 15 or 5 mg/kg
Administration: Intraperitoneal injection; 15 or 5 mg/kg; once every other day; 4 times
Result: Reduced tumor mass by 45.7% and 16.9% at 15 and 5 mg/kg, respectively.
Showed no sign of toxicity and no decreasement in animal body weight.
Molecular Weight

371.38

Formula

C20H21NO6

CAS No.
SMILES

CCOC1=CC2=C(C(C(C3=CC(OC)=C(C(OC)=C3)OC)=O)=C(O2)N)C=C1

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Tubulin polymerization-IN-13
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HY-146209
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